In vitro Antioxidant Properties of Novel β3-Adrenoceptor Agonists Bearing Benzenesulfonamide Fragment

Authors

  • Lubica Sichrovska
  • Ivan Malik
  • Eva Sedlarova
  • Jozef Csollei
  • Jan Muselik

Keywords:

Antioxidant properties, ?3-adrenoceptor agonists, lipophilicity

Abstract

As an extension of our research, the in vitro antioxidant efficiency of perspective agonists of
β3-adrenoceptors structurally based on the aryloxypropanolamine pharmacophore, chemically 3-{4-
[(alkoxycarbonyl)amino]phenoxy}-N-{2-[4-(aminosulfonyl)phenyl]ethyl}-2-hydroxypropan-1-ammonium chlorides,
was investigated. The potential of evaluated compounds to reduce relatively stable 2,2-diphenyl-1-picrylhydrazyl
(DPPH) radicals in the spectrophotometric tests was dependent on the length of the alkyl substituent
of alkoxycarbonylamino moiety directly attached to phenyl ring. The elongation of given string was accompanied by
the increase in the effectiveness. From the entire analyzed set, the compound containing butoxycarbonylamino group
has been able to act most markedly as the reduction agent towards the DPPH radicals showing the percentage of the
DPPH reduction (% DPPH) of 11.34±0.02. On the other hand, the tested derivative has shown approximately
ninefold decrease in the efficiency compared to applied Trolox standard, a water-soluble analogue of vitamin E, with
its %DPPH=95.45±0.02.

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